护肝颗粒中五味子醇甲含量测定方法研究

目的:制定护肝颗粒中五味子醇甲含量测定方法。方法:采用HPLC法,色谱柱为C18,流动相为甲醇-水(63:37);检测波长250nm。结果:五味子醇甲在0.02052μg~0.513μg范围内,进样量与峰面积线性关系良好(r=1.0000)。加样回收率为98.7%(RSD为0.6%)。结论:此方法准确可靠、重复性好,可用于护肝颗粒中五味子醇甲的含量测定。     

HPLC法同时测定护肝片中五味子醇甲、五味子甲素、五味子乙素的含量

目的:对护肝片含量测定方法进行修订,并建立同时测定护肝片中五味醇甲、五味子甲素、五味子乙素含量的方法。方法:色谱柱为C18柱,流动相为甲醇-水(梯度洗脱),流量1.0 mL.min-1;检测波长220 nm。结果:五味子醇甲、五味子甲素、五味子乙素的线性范围分别为0.99～4.95μg,0.39～1.96μg,0.34～1.71μg;平均回收率分别为99.2%、96.4%、99.1%;RSD分别为1.2%、2.5%、1.5%(n=6)。结论:该方法操作简便、准确,重复性好,可用于护肝片质量控制。     

高效液相色谱法测定北五味子藤茎超临界提取物中五味子甲素、五味子乙素和五味子醇甲的含量

目的 高效液相色谱(HPLC)法测定北五味子藤茎超临界提取物中五味子甲素、五味子乙素、五味子醇甲的含量.方法 采用ODS-C18(5 μm,4.6 × 250 mm),以甲醇-水(75:25)为流动相,流速:1.0 ml/min,检测波长为254 nm.结果 五味子甲素、五味子乙素、五味子醇甲的线性范围分别为0.1～2.0μg/(r=0.9994)、0.1～2.0μg(r=0.9997)、0.12～2.0μg(r=0.9992),平均加样回收率分别为99.03%、103.60%、99.80%,RSD分别为1.72%、2.09%、1.33%(n=5).结论 本方法简便准确、重现性好,能有效测定北五味子藤茎超临界提取物中五味子甲素、五味子乙素、五味子醇甲的含量.     

护肝丸中五味子醇甲的含量测定研究

目的建立HPLC测定五味子醇甲含量的方法。方法以反相高效液相法测定五味子醇甲的含量。色谱柱:Hanbon LichrospherC1(8250×4.6mm×5μm);流动相:甲醇-水(63∶37);检测波长:251nm;结果五味子醇甲在0.1051～2.102μg浓度范围内线性关系良好;(r=0.9999,n=7)平均加样回收率为97.03%,RSD为1.02%。结论该方法快速,简便,准确,重复性好。     

HPLC法测定参芪消渴胶囊中五味子醇甲的含量

目的:建立高效液相色谱法(HPLC)测定参芪消渴胶囊中五味子醇甲的含量.方法:采用Agilent HC-C18(4.6 mm×250 mm,5μm)色谱柱;流动相为以甲醇为流动相A,水为流动相B,进行梯度洗脱;检测波长为250 nm,结果:五味子醇甲在0.0924～2.31μg范围内线性关系良好(r=0.999 9),平均回收率为99.58%,RSD为0.92%(n＝6).结论:本方法可作为参芪消渴胶囊的质量控制方法.     

HPLC法测定复方五味子补肾颗粒中的五味子醇甲的含量

目的建立复方五味子补肾颗粒中五味子醇甲的含量测定方法。方法采用高效液相色谱法测定复方五味子补肾颗粒中五味子醇甲的含量。Welch Materials C18色谱柱(4.6 mm×250 mm,5μm);甲醇-水(70∶30)为流动相;流速:1.0 ml.min-1;柱温25℃。结果在高效液相色谱法图中,五味子醇甲与其它组份分离良好,线性范围为0.024 4～0.244 g.L-1,其回归方程为:Y=39 648.426X+51.18,r=0.999 9(n=6),线性良好为0.024 4～0.244 g.L-1,平均加样回收率为99.46%(RSD=0.54%)。结论该方法可以很好的用于控制复方五味子补肾颗粒的质量。     

高效液相色谱法同时测定五味护肝胶囊中五味子醇甲、五味子甲素和五味子乙素含量

目的 建立同时测定五味护肝胶囊中五味子醇甲、五味子甲素和五味子乙素含量的高效液相色谱法.方法 采用高效液相色谱法,色谱柱为Waters sunfire TMC18柱(150mm×4.6mm,5 μm);以乙腈-水(56:32)为流动相,流速为1.0mL/min,检测波长为250 nm.结果 五味子醇甲进样量的线性范围为0.087 04～0.696 32 μg,r=0.999 98,平均回收率为103.40%,RSD为1.42%(n:6);五味子甲素进样量线性范围为0.018 304～0.146 43μg,r=0.999 98,平均回收率为97.45%,RSD为0.88%(n=6);五味子乙素进样量的线性范围为0.040 80～0.326 4 μg,r=0.999 96,平均加样回收率为95.88%,RSD为0.76%(n=6).结论 该方法简便、快速、准确,重现性好,可作为该制剂的含量测定方法.     

HPLC法测定生脉饮中五味子醇甲的含量

目的:建立一种生脉饮中五味子醇甲的高效液相色谱测定方法.方法:Hypersilbds(250mm×4.6mm,5μm)为色谱柱:用甲醇-水(62:38)为流动相;以外标法按峰面积计算.结果:五味子醇甲在8.4-84μml范围呈良好的线性关系,该法回收率为99.62%.结论:该法简便快捷,结果准确,可用于生脉饮中五味子醇甲的含量测定和质量控制.     

七味都气丸中五味子醇甲的含量测定

目的:建立HPLC法七味都气丸中五味子醇甲含量的测定方法。方法:采用高效液相色谱法,色谱柱:钻石ODS柱(200 mm×4.6mm,5μm)。流动相:甲醇-水(64:36);流速为1.0ml·min~(-1);检测波长为250 nm;室温。结果:五味子醇甲的线性范围是0.12～1.48μg,r=0.999 9。平均加样回收率为98.2%,RSD=1.0%(n=9)。结论:该法可以用于测定七味都气丸中五味子醇甲的含量。     

肝宝胶囊中五味子醇甲的含量测定

目的:探讨肝宝胶囊中五味子醇甲的含量测定方法.方法:用高效液相色谱法测定了五味子醇甲的含量.结果:五味子醇甲线性范围是 0.17～ 0.85 μ g; 平均加样回收率为 98.80%,RSD=1.03%(n=5).结论:高效液相色谱法准确可靠,可用于该药的质量控制.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.